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Th1067 details
Primary information
ID1409
ThPP IDTh1067
Therapeutic Peptide/Protein NameDaptomycin
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1620.6706
Chemical FormulaC72H101N17O26
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life7 days
DescriptionDaptomycin is a lipopeptide antibiotic that kills susceptible gram positive bacteria by disrupting their membrane potential. It is a naturally-occurring compound found in the soil bacterium <i>Streptomyces roseosporus</i>. Antibiotics are used in the treatment of infections caused by bacteria. They work by killing bacteria or preventing their growth. Daptomycin will not work for colds, flu, or other virus infections. It was approved in September 2003 for the treatment of complicated skin and soft tissue infections. It has a safety profile similar to other agents commonly administered to treat gram-positive infections.
Indication/DiseaseFor the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms.
PharmacodynamicsDaptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant <i>Staphylococcus aureus</i>), streptococci and corynebacteria. Daptomycin is derived from the fermentation product of Streptomyces roseosporus.
Mechanism of ActionDaptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the cell membrane. This binding causes rapid depolarisation, resulting in a loss of membrane potential leading to inhibition of protein, DNA and RNA synthesis, which results in bacterial cell death. The bactericidal activity of daptomycin is concentration-dependent. There is in vitro evidence of synergy with β-lactam antibiotics.
ToxicityN.A.
MetabolismMinor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified.
AbsorptionN.A.
Volume of Distribution0.1 L/Kg [healthy adult subjects]
ClearanceN.A.
CategoriesN.A.
Patents NumberUS6468967
Date of Issue25/09/03
Date of Expiry25/09/23
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameCUBICIN
CompanyCubist Pharmaceuticals, Inc
Brand DiscriptionCUBICIN contains daptomycin, a cyclic lipopeptide antibacterial agent derived from the fermentation of Streptomyces roseosporus.The empirical formula is C72H101N17O26; the molecular weight is 1620.67
Prescribed forComplicated skin and skin structure infections (cSSSI), Staphylococcus aureus bloodstream infections (bacteremia), including those with right-sided infective endocarditis, caused by methicillin-susceptible and methicillin-resistant isolates
Chemical NameN-decanoyl-L-tryptophyl-Dasparaginyl-L-aspartyl-L-threonylglycyl-L-ornithyl-L-aspartyl-D-alanyl-L-aspartylglycyl-Dseryl-threo-3-methyl-L-glutamyl-3-anthraniloyl-L-alanine ε1-lactone
FormulationCUBICIN contains 500 mg of daptomycin and reconstituted with 0.9% sodium chloride injection. The only inactive ingredient is sodium hydroxide, which is used in minimal quantities for pH adjustment.
Physcial AppearanceCUBICIN is a Sterile, preservative-free, pale yellow to light brown, lyophilized cake containing approx 500 mg of daptomycin
Route of AdministrationIntravenous (Intravenous) Injection
Recommended DosageCUBICIN 4 mg/kg should be administered intravenously in 0.9% sodium chloride injection once every 24 hours for 7 to 14 days. Staphylococcus aureus Bloodstream Infections (Bacteremia) - CUBICIN 6 mg/kg should be administered intravenously in 0.9% sodium chloride injection once every 24 hours for 2 to 6 weeks.
ContraindicationCUBICIN is contraindicated in patients with known hypersensitivity to daptomycin
Side Effectsfatigue, weakness, rigors, flushing, hypersensitivity, leukocytosis, thrombocytopenia, thrombocytosis, eosinophilia, increased International Normalized Ratio (INR), supraventricular arrhythmia, eczema, abdominal distension, stomatitis, jaundice, increased serum lactate dehydrogenase, hypomagnesemia, increased serum bicarbonate, electrolyte disturbance, myalgia, muscle cramps, muscle weakness, arthralgia, vertigo, mental status change, paresthesia, taste disturbance, eye irritation
Useful Linkhttp://www.rxlist.com/cubicin-drug.htm http://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a7975871-46a6-4e9b-a8b5-38bfcb465f0e
PubMed ID16805723, 11020247, 1318678
3-D StructureN.A.
Primary information
ID1410
ThPP IDTh1067
Therapeutic Peptide/Protein NameDaptomycin
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1620.6706
Chemical FormulaC72H101N17O26
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life8 days
DescriptionDaptomycin is a lipopeptide antibiotic that kills susceptible gram positive bacteria by disrupting their membrane potential. It is a naturally-occurring compound found in the soil bacterium <i>Streptomyces roseosporus</i>. Antibiotics are used in the treatment of infections caused by bacteria. They work by killing bacteria or preventing their growth. Daptomycin will not work for colds, flu, or other virus infections. It was approved in September 2003 for the treatment of complicated skin and soft tissue infections. It has a safety profile similar to other agents commonly administered to treat gram-positive infections.
Indication/DiseaseFor the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms.
PharmacodynamicsDaptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant <i>Staphylococcus aureus</i>), streptococci and corynebacteria. Daptomycin is derived from the fermentation product of Streptomyces roseosporus.
Mechanism of ActionDaptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the cell membrane. This binding causes rapid depolarisation, resulting in a loss of membrane potential leading to inhibition of protein, DNA and RNA synthesis, which results in bacterial cell death. The bactericidal activity of daptomycin is concentration-dependent. There is in vitro evidence of synergy with β-lactam antibiotics.
ToxicityN.A.
MetabolismMinor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified.
AbsorptionN.A.
Volume of Distribution0.1 L/Kg [healthy adult subjects]
ClearanceN.A.
CategoriesN.A.
Patents NumberUSRE39071
Date of Issue16/06/00
Date of Expiry16/06/20
Drug InteractionN.A.
TargetN.A.
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID16805723, 11020247, 1318678
3-D StructureN.A.
Primary information
ID1411
ThPP IDTh1067
Therapeutic Peptide/Protein NameDaptomycin
SequenceN.A. view full sequnce in fasta
Functional ClassificationIIa
Molecular Weight1620.6706
Chemical FormulaC72H101N17O26
Isoelectric PointN.A.
HydrophobicityN.A.
Melting Point (℃)N.A.
Half Life9 days
DescriptionDaptomycin is a lipopeptide antibiotic that kills susceptible gram positive bacteria by disrupting their membrane potential. It is a naturally-occurring compound found in the soil bacterium <i>Streptomyces roseosporus</i>. Antibiotics are used in the treatment of infections caused by bacteria. They work by killing bacteria or preventing their growth. Daptomycin will not work for colds, flu, or other virus infections. It was approved in September 2003 for the treatment of complicated skin and soft tissue infections. It has a safety profile similar to other agents commonly administered to treat gram-positive infections.
Indication/DiseaseFor the treatment of complicated skin and skin structure infections caused by susceptible strains of Gram-positive microorganisms.
PharmacodynamicsDaptomycin is a 13 member amino acid cyclic lipopeptide antibiotic active against Gram-positive bacteria only. It has proven in vitro activity against enterococci (including glycopeptide-resistant Enterococci (GRE)), staphylococci (including methicillin-resistant <i>Staphylococcus aureus</i>), streptococci and corynebacteria. Daptomycin is derived from the fermentation product of Streptomyces roseosporus.
Mechanism of ActionDaptomycin appears to bind or insert into the outer membrane of gram positive bacteria. The binding and integration of daptomycin into the cell membrane is calcium dependent. Calcium ions cause a conformational change in daptomycin, augmenting its amphipathicity (hydrophilic head group and hydrophobic tail group), leading to incorporation into the cell membrane. This binding causes rapid depolarisation, resulting in a loss of membrane potential leading to inhibition of protein, DNA and RNA synthesis, which results in bacterial cell death. The bactericidal activity of daptomycin is concentration-dependent. There is in vitro evidence of synergy with β-lactam antibiotics.
ToxicityN.A.
MetabolismMinor amounts of three oxidative metabolites and one unidentified compound have been detected in urine. The site of metabolism has not been identified.
AbsorptionN.A.
Volume of Distribution0.1 L/Kg [healthy adult subjects]
ClearanceN.A.
CategoriesN.A.
Patents NumberCA2344318
Date of Issue05/07/10
Date of Expiry25/09/23
Drug InteractionN.A.
TargetB-lymphocyte antigen CD20,Low affinity immunoglobulin gamma Fc region receptor III-B,Complement C1r subcomponent,Complement C1q subcomponent subunit A,Complement C1q subcomponent subunit B,Complement C1q subcomponent subunit C,Low affinity immunoglobulin gamma Fc region receptor III-A,Complement C1s subcomponent,High affinity immunoglobulin gamma Fc receptor I,Low affinity immunoglobulin gamma Fc region receptor II-a,Low affinity immunoglobulin gamma Fc region receptor II-b,Low affinity immunoglobulin gamma Fc region receptor II-c
Information of corresponding available drug in the market
Brand NameN.A.
CompanyN.A.
Brand DiscriptionN.A.
Prescribed forN.A.
Chemical NameN.A.
FormulationN.A.
Physcial AppearanceN.A.
Route of AdministrationN.A.
Recommended DosageN.A.
ContraindicationN.A.
Side EffectsN.A.
Useful LinkN.A.
PubMed ID16805723, 11020247, 1318678
3-D StructureN.A.